AU-15330|cas:2380274-50-8|西域试剂

AU-15330,99.57%

产品编号：Bellancom-145388| CAS NO：2380274-50-8| 分子式：C₃₉H₄₉N₉O₅S| 分子量：755.93

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货号	价格	库存与货期
Bellancom-145388	￥4200.00	杭州北京（现货）
Bellancom-145388	￥6500.00	杭州北京（现货）
Bellancom-145388	￥13000.00	杭州北京（现货）

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AU-15330

产品介绍

AU-15330 是 SWI/SNF ATP 酶亚基 SMARCA2 和 SMARCA4 的蛋白水解靶向嵌合体 (PROTAC) 降解剂。AU-15330 在前列腺癌异种移植模型中诱导有效抑制肿瘤生长，并与 AR 拮抗剂 enzalutamide 协同作用。AU-15330 在去势抵抗性前列腺癌 (CRPC) 模型中诱导疾病缓解而无毒性。

生物活性

AU-15330 is a proteolysis-targeting chimera (PROTAC) degrader of the SWI/SNF ATPase subunits, SMARCA2 and SMARCA4. AU-15330 induces potent inhibition of tumour growth in xenograft models of prostate cancer and synergizes with the AR antagonist enzalutamide. AU-15330 induces disease remission in castration-resistant prostate cancer (CRPC) models without toxicity.

体外研究

体内研究

AU-15330 (10 and 30 mg/kg; i.v.; 5 days per week for 3 weeks) shows no evident toxicity in immuno-competent mice.
AU-15330 (60 mg/kg with or without 10 mg/kg enzalutamide; i.v.; 3 days per week; p.o.; 5 days per week for 5 weeks) leads to potent inhibition of tumour growth, triggering disease regression in more than 20% of animals. Combinatorial regimen induced the most potent anti-tumour effect, with regression in all animals.
AU-15330 (60 mg/kg with or without 10 mg/kg enzalutamide; i.v.; 3 days per week; p.o.; 5 days per week for 5 weeks) strongly inhibits the growth of C4-2B cell line-derived CRPC xenografts in intact mice as a single agent and synergized with enzalutamide.
AU-15330 (60 mg/kg with or without 10 mg/kg enzalutamide; i.v.; 3 days per week; p.o.; 5 days per week for 5 weeks) combines with enzalutamide induces significant tumour growth inhibition, causing regression in more than 30% of animals in the modle of CRPC variant of the MDA-PCa-146-12 PDX by tumour implantation into castrated mice.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Six-week-old male CB17 severe combined immunodeficiency (SCID) mice
Dosage:	10 and 30 mg/kg
Administration:	i.v. (5 days per week for 3 weeks)
Result:	Showed no evident toxicity in immuno-competent mice.

Animal Model:	VCaP castration-resistant tumour model (six-week-old male CB17 severe combined immunodeficiency (SCID) mice)
Dosage:	60 mg/kg with or without 10 mg/kg enzalutamide
Administration:	i.v. (3 days per week); p.o. (5 days per week for 5 weeks)
Result:	Resulted inhibition of tumor growth and triggered disease regression in more than 20% of animals. Combinatorial regimen induced the most potent anti-tumour effect, with regression in all animals.

Animal Model:	C4-2B non-castrated tumour model (six-week-old male CB17 severe combined immunodeficiency (SCID) mice)
Dosage:	60 mg/kg with or without 30 mg/kg enzalutamide
Administration:	i.v. (3 days per week); p.o. (5 days per week for 4 weeks)
Result:	Strongly inhibited the growth of C4-2B cell line-derived CRPC xenografts in intact mice as a single agent and synergized with enzalutamide.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Six-week-old male CB17 severe combined immunodeficiency (SCID) mice
Dosage:	10 and 30 mg/kg
Administration:	i.v. (5 days per week for 3 weeks)
Result:	Showed no evident toxicity in immuno-competent mice.

Animal Model:	VCaP castration-resistant tumour model (six-week-old male CB17 severe combined immunodeficiency (SCID) mice)
Dosage:	60 mg/kg with or without 10 mg/kg enzalutamide
Administration:	i.v. (3 days per week); p.o. (5 days per week for 5 weeks)
Result:	Resulted inhibition of tumor growth and triggered disease regression in more than 20% of animals. Combinatorial regimen induced the most potent anti-tumour effect, with regression in all animals.

Animal Model:	C4-2B non-castrated tumour model (six-week-old male CB17 severe combined immunodeficiency (SCID) mice)
Dosage:	60 mg/kg with or without 30 mg/kg enzalutamide
Administration:	i.v. (3 days per week); p.o. (5 days per week for 4 weeks)
Result:	Strongly inhibited the growth of C4-2B cell line-derived CRPC xenografts in intact mice as a single agent and synergized with enzalutamide.

性状

Solid

溶解性数据

In Vitro:

DMSO : 140 mg/mL (185.20 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.3229 mL	6.6144 mL	13.2287 mL
5 mM	0.2646 mL	1.3229 mL	2.6457 mL
10 mM	0.1323 mL	0.6614 mL	1.3229 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 3.5 mg/mL (4.63 mM); Clear solution

此方案可获得 ≥ 3.5 mg/mL (4.63 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 35.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 3.5 mg/mL (4.63 mM); Clear solution

此方案可获得 ≥ 3.5 mg/mL (4.63 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 35.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 3.5 mg/mL (4.63 mM); Clear solution

此方案可获得 ≥ 3.5 mg/mL (4.63 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 35.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。